UGT Inhibition

Glucuronidation caused by uridine 5'-diphospho-glucuronosyltransferases (UGT) is an important pathway for drug metabolism in humans and other mammals. The inhibition of UGT, although less often observed than CYP inhibition, is a clinically significant form of drug-drug interactions and may lead to toxicity. Therefore, the elucidation of UGT inhibition is recommended by the regulatory authorities especially in cases where direct glucuronidation is one of the major elimation routes for the new chemical entity.